Theophylline

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Euphyllin Retard, Respicur, Theospirex Retard, Unifyl Retard; Belgium: Euphyllin, Theolair, Xanthium; Bulgaria: Teotard; Cyprus: Theo-Dur, Uniphyllin Continus; Czech Republic: Afonilum, Euphyllin, Theoplus; Denmark: Nuelin Retard, Theo-Dur, Unixan; Estonia: Retafyllin, Teotard; Finland: Nuelin, Retafyllin, Theofol; France: Dilatrane, Euphylline, Pneumogeine, Tedralan, Theostat, Xanthium; Germany: Aerobin, Afonilum, Bronchoparat, Bronchoretard, Contiphyllin, Euphyllin, Euphylong, Pulmo-Timelets, Pulmotractan, Solosin, Theo-CT, Theomol, Theophyllin, Uniphyllin; Greece: Bronchogeril, Theo-Dur, Theoplus, Uniphyllin; Hungary: Egifilin, Euphylong; Ireland: Nuelin, Uniphyllin Continus, Zepholin SR; Italy: Aminomal Elisir, Diffumal, Euphyllina, Respicur, Theo-Dur, Theolair; Latvia: Retafyllin, Teotard; Lithuania: Teotard; Luxembourg: Pediaphyllin, Theo-2, Theo-Dur, Theolair, Theophyllin, Theostat, Xanthium; Malta: Nuelin; Netherlands: Theolair; Poland: Afonilum, Euphyllin, Theo-Dur, Theophyllinum, Theoplus, Theospirex, Theovent; Portugal: Eufilina, Unicontin; Romania: Teofilina, Teotard, Theo SR; Slovakia: Afonilum, Euphyllin, Theoplus; Slovenia: Teotard; Spain: Elixifilin, Eufilina, Histafilin, Pulmeno, Teromol, Theo-Dur, Theolair, Theoplus; Sweden: Teofyllamin, Theo-Dur; UK: Nuelin, Slo-Phyllin, Uniphyllin Continus.

North America

Canada: Apo-Theo-LA, Novo-Theophyl, Pulmophylline, Theolair, Theophylline, Uniphyl; USA: Elixophyllin, Theo-24, Theochron, Theolair, Theophylline, Uniphyl.

Latin America

Argentina: Drilyna, Nefoben, Teofilina, Teosona; Brazil: Codrinan, Talofilina, Teofilab, Teolong, Teophyl, Teoston; Mexico: Elixofilina, Fluidasa.

Asia

Japan: Ardephyllin, Cylmin, Flemphyline, Sekiroid, Slo-Bid, Telbans, Teofurmate, Terdan, Theodrip, Theodur, Theolong, Theo Slow, Unicon, Uniphyl.

Drug combinations

Theophylline and Ambroxol

Theophylline and Aminophylline

Theophylline and Dexamethasone

Theophylline and Ephedrine

Theophylline and Ethylenediamine

Theophylline and Guaifenesin

Theophylline, Butobarbital, and Ephedrine

Theophylline, Caffeine, and Ephedrine

Chemistry

Theophylline: C~7~H~8~N~4~O~2~ H~2~O. Mw: 198.18. (1) 1H-Purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-, monohydrate; (2) Theophylline monohydrate. CAS-5967-84-0; CAS-58-55-9 (anhydrous).

Theophylline Sodium Glycinate: (1) Glycine, mixt. with 3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione, monosodium salt; (2) Theophylline sodium mixture with glycine. CAS-8000-10-0.

Pharmacologic Category

Anorexigenic Agents and Respiratory and Cerebral Stimulants, Miscellaneous. Respiratory Smooth Muscle Relaxants; Theophylline Derivative. (ATC-Code: R03DA04).

Mechanism of action

Causes bronchodilatation, diuresis, CNS and cardiac stimulation, and gastric acid secretion by blocking phosphodiesterase (PDE) which increases tissue concentrations of cyclic adenine monophosphate (cAMP), which in turn promotes catecholamine stimulation of lipolysis, glycogenolysis, and gluconeogenesis and induces release of epinephrine from adrenal medulla cells.

Therapeutic use

Treatment of symptoms and reversible airway obstruction due to chronic asthma, or other chronic lung diseases. Apnea of prematurity.

Pregnancy and lactiation implications

Theophylline crosses placenta; adverse effects may be seen in newborn. Use generally safe when used at recommended doses, however maternal adverse events may be increased and efficacy may be decreased in pregnant women. Theophylline metabolism may change during pregnancy. Enters breast milk, compatible with lactation.

Unlabeled use

Contraindications

Hypersensitivity to theophylline or any component of the formulation. Premixed injection may contain corn-derived dextrose and is contraindicated in allergy to corn-related products.

Warnings and precautions

Theophylline toxicity (e.g. persistent, repetitive vomiting), might be developed. Theophylline clearance may be decreased in acute pulmonary edema, congestive heart failure, cor pulmonale, fever, hepatic disease, acute hepatitis, cirrhosis, hypothyroidism, sepsis with multiorgan failure, and shock. Clearance may also be decreased in neonates, infants <3 months of age with decreased renal function, children <1 year of age, the elderly >60 years of age, and patients following cessation of smoking. Use with caution in tachyarrhythmias since use may exacerbate these arrhythmias, in hyperthyroidism (may be exacerbated with use), in peptic ulcer disease (may be exacerbated with use), and in history of seizure disorder (may be exacerbated with use).

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